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1202580-59-3

中文名稱 CAY10618
英文名稱 CAY10618
CAS 1202580-59-3
分子式 C27H29N5O
分子量 439.55
MOL 文件 1202580-59-3.mol
1202580-59-3 結構式 1202580-59-3 結構式

基本信息

中文別名
化合物 T15412
英文別名
GPP 78
CAY10618
CAY10618 Exclusive
N-(2-phenylphenyl)-8-(4-pyridin-3-yltriazol-1-yl)octanamide
1H-1,2,3-Triazole-1-octanaMide, N-[1,1'-biphenyl]-2-yl-4-(3-pyridinyl)-

物理化學性質

密度1.15±0.1 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度DMF: 10 mg/ml; DMSO: 10 mg/ml; DMSO:PBS(pH 7.2) (1:3): 0.25 mg/ml; Ethanol: 10 mg/ml
酸度系數(shù)(pKa)14.80±0.70(Predicted)
形態(tài)Liquid
顏色Colorless to light yellow

常見問題列表

生物活性
GPP78 (CAY10618) 是一種有效的煙酰胺磷酸核糖轉移酶 (Nampt) 抑制劑,對 NAD 消耗的 IC50 為 3 nM。GPP78 通過誘導自噬對神經母細胞瘤細胞 SH-SY5Y 具有毒性,IC50 為 3.8 nM。GPP78 具有抗癌和抗炎作用。
靶點

Nampt;
Autophagy

體外研究

GPP78 (Compound 8; 10 nM; 24-40 hours; SH-SY5Y cells) treatment with cells, punctate staining of LC3-II and the formation of autophagolysosomes are observable. LC3-II is membrane-bound and is present in autophagosomes.
GPP78 (Compound 8) inhibits the growth of most cell lines tested, with nanomolar potency (GI 50 ) in cell lines derived from leukemia, lung, CNS, colon, melanoma, ovarian, renal, and prostate cancers. GPP78 appears truly cytotoxic in melanoma cell lines, while in the others it is mainly cytostatic.

Western Blot Analysis

Cell Line: SH-SY5Y cells
Concentration: 10 nM
Incubation Time: 24 hours, 40 hours
Result: Punctate staining of LC3-II and the formation of autophagolysosomes were observable.
體內研究

GPP78 (10 mg/kg; intraperitoneal injection; daily; 1 hour or 6 hours after SCI; for 19 days; male adult CD1 mice) treatment reduces the severity of spinal cord trauma in SCI mice.

Animal Model: Male adult CD1 mice (25-30 g) with spinal cord injury (SCI)
Dosage: 10 mg/kg
Administration: Intraperitoneal injection; daily; 1 hour or 6 hours after SCI; for 19 days
Result: Significantly reduced the demyelination associated with SCI. And significantly ameliorated the functional deficits induced by SCI.
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